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Protein concentrations were determined using the Pierce BCA Protein Assay kit (NCI1059CH, Thermo, Waltham, MA, USA) and then adjusted to the same level

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The X-ray-derived data of small molecular fragments in complex with TGR used in this study to design the compounds here described are available in the PDB under accession codes 6FTC, 6FMU, 6FMZ, 6FP4, 2X99, 2X8G, 2X8H, 6ZST, 6ZP3, 6ZLP, 6ZLB, 7B02, 7NPX, 2V6O, 6RTJ, 6RTO, 6RTM, and 3H4K